Small molecules are powerful pharmacological tools to dissect biological events. There is now considerable interest in expanding efforts to identify and use small molecules targeting proteins encoded in the genomes of humans and pathogenic organisms. Integration of the principles of molecular pharmacology with contemporary high-throughput and high-content screening technologies is essential for the success of these discovery activities. We present some of the challenges and opportunities provided by the Molecular Library Screening Centers Network (MLSCN), which is a National Institutes of Health Roadmap Initiative.
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